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Drug Delivery

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https://www.readbyqxmd.com/read/28195032/ph-responsive-carriers-for-oral-drug-delivery-challenges-and-opportunities-of-current-platforms
#1
Lin Liu, WenDong Yao, YueFeng Rao, XiaoYang Lu, JianQing Gao
Oral administration is a desirable alternative of parenteral administration due to the convenience and increased compliance to patients, especially for chronic diseases that require frequent administration. The oral drug delivery is a dynamic research field despite the numerous challenges limiting their effective delivery, such as enzyme degradation, hydrolysis and low permeability of intestinal epithelium in the gastrointestinal (GI) tract. pH-Responsive carriers offer excellent potential as oral therapeutic systems due to enhancing the stability of drug delivery in stomach and achieving controlled release in intestines...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28181841/surface-density-of-polyarginine-influence-the-size-zeta-potential-cellular-uptake-and-tissue-distribution-of-the-nanostructured-lipid-carrier
#2
Mingshuang Sun, Zhihong Zhu, Huixin Wang, Cuiyan Han, Dandan Liu, Lei Tian, Xinggang Yang, Weisan Pan
Poly-arginines are strong tools to elevate the cellular uptake of nanopreparations. To learn the influence of poly-arginine (RRRRRRRR, R8) density on a series of properties of nanostructured lipid carrier (NLC), we build six R8 modified NLCs with different R8 densities (nR-NLC, where n represents the R8 ratio) by fusion-emulsion method with the aid of stearyl-R8. The pharmaceutical characteristics like size, zeta potential and in vitro drug release, cellular uptake, cytotoxicity to A549 cells and tissue distribution in S180 tumor-bearing mice of the six nR-NLCs are all investigated...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28181840/transdermal-delivery-of-isoniazid-and-rifampin-in-guinea-pigs-by-electro-phonophoresis
#3
Suting Chen, Yi Han, Daping Yu, Fengmin Huo, Fen Wang, Yunxu Li, Lingling Dong, Zhidong Liu, Hairong Huang
Electro-phonophoresis (EP) has been used as a drug delivery approach in clinical fields. The objective of the present study is to evaluate the skin permeability of isoniazid and rifampin in guinea pigs by EP to provide reference basis for clinical applications of such transdermal delivery system in the treatment of patients with superficial tuberculosis. Isoniazid and rifampin solutions were delivered transdermally with or without EP in health guinea pigs for 0.5 h. Local skin and blood samples were collected serially at 0, 1/2, 1, 2, 4, 6 and 24 h after dosing...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28181839/anhydrous-reverse-micelle-nanoparticles-new-strategy-to-overcome-sedimentation-instability-of-peptide-containing-pressurized-metered-dose-inhalers
#4
Zhengwei Huang, Han Wu, Beibei Yang, Longkai Chen, Ying Huang, Guilan Quan, Chune Zhu, Xing Li, Xin Pan, Chuanbin Wu
The objective of this study was to develop a novel anhydrous reverse micelle nanoparticles (ARM-NPs) system to overcome the sedimentation instability of peptide-containing pressurized metered-dose inhalers (pMDIs). A bottom-up method was utilized to fabricate ARM-NPs. Tertiary butyl alcohol (TBA)/water system, freeze-drying and lipid inversion method were successively used to produce the ARM-NPs for pMDI. Various characteristics of ARM-NPs were investigated including particle size, morphology, secondary structure of the peptide drug, aerosolization properties and storage stability...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28181835/irinotecan-encapsulated-double-reverse-thermosensitive-nanocarrier-system-for-rectal-administration
#5
Fakhar Ud Din, Ju Yeon Choi, Dong Wuk Kim, Omer Mustapha, Dong Shik Kim, Raj Kumar Thapa, Sae Kwang Ku, Yu Seok Youn, Kyung Taek Oh, Chul Soon Yong, Jong Oh Kim, Han-Gon Choi
Intravenously administered for the treatment of rectum cancer, irinotecan produces severe side effects due to very high plasma concentrations. A novel irinotecan-encapsulated double reverse thermosensitive nanocarrier system (DRTN) for rectal administration was developed as an alternative. The DRTN was fabricated by dispersing the thermosensitive irinotecan-encapsulated solid lipid nanoparticles (SLN) in the thermosensitive poloxamer solution. Its gel properties, pharmacokinetics, morphology, anticancer activity and immunohistopathology were assessed after its rectal administration to rats and tumor-bearing mice...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28181832/a-tumor-targeting-crgd-egfr-sirna-conjugate-and-its-anti-tumor-effect-on-glioblastoma-in-vitro-and-in-vivo
#6
Shuai He, Bohong Cen, Lumin Liao, Zhen Wang, Yixin Qin, Zhuomin Wu, Wenjie Liao, Zhongyi Zhang, Aimin Ji
The epidermal growth factor receptor (EGFR) is an important anti-tumor target. The development of novel molecular-targeted anti-tumor drugs that can target the interior of tumor cells and specifically silence EGFR expression is valuable and promising. In this work, a promising anti-tumor conjugate comprising methoxy-modified EGFR siRNA and cyclic arginine-glycine-aspartic acid (cRGD) peptides, which selectively bind to αvβ3 integrins, was synthesized and examined. To prepare cRGD-EGFR siRNA (cRGD-siEGFR), cRGD was covalently conjugated to the 5'-end of an siRNA sense strand using a thiol-maleimide linker...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28181831/basic-concepts-and-recent-advances-in-nanogels-as-carriers-for-medical-applications
#7
Iordana Neamtu, Alina Gabriela Rusu, Alina Diaconu, Loredana Elena Nita, Aurica P Chiriac
Nanogels in biomedical field are promising and innovative materials as dispersions of hydrogel nanoparticles based on crosslinked polymeric networks that have been called as next generation drug delivery systems due to their relatively high drug encapsulation capacity, uniformity, tunable size, ease of preparation, minimal toxicity, stability in the presence of serum, and stimuli responsiveness. Nanogels show a great potential in chemotherapy, diagnosis, organ targeting and delivery of bioactive substances...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28181829/marked-augmentation-of-plga-nanoparticle-induced-metabolically-beneficial-impact-of-%C3%AE-oryzanol-on-fuel-dyshomeostasis-in-genetically-obese-diabetic-ob-ob-mice
#8
Chisayo Kozuka, Chigusa Shimizu-Okabe, Chitoshi Takayama, Kaku Nakano, Hidetaka Morinaga, Ayano Kinjo, Kotaro Fukuda, Asuka Kamei, Akihito Yasuoka, Takashi Kondo, Keiko Abe, Kensuke Egashira, Hiroaki Masuzaki
Our previous works demonstrated that brown rice-specific bioactive substance, γ-oryzanol acts as a chaperone, attenuates exaggerated endoplasmic reticulum (ER) stress in brain hypothalamus and pancreatic islets, thereby ameliorating metabolic derangement in high fat diet (HFD)-induced obese diabetic mice. However, extremely low absorption efficiency from intestine of γ-oryzanol is a tough obstacle for the clinical application. Therefore, in this study, to overcome extremely low bioavailability of γ-oryzanol with super-high lipophilicity, we encapsulated γ-oryzanol in polymer poly (DL-lactide-co-glycolide) (PLGA) nanoparticles (Nano-Orz), and evaluated its metabolically beneficial impact in genetically obese-diabetic ob/ob mice, the best-known severest diabetic model in mice...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28181828/synthesis-of-sericin-based-conjugates-by-click-chemistry-enhancement-of-sunitinib-bioavailability-and-cell-membrane-permeation
#9
Luca Scrivano, Domenico Iacopetta, Maria Stefania Sinicropi, Carmela Saturnino, Pasquale Longo, Ortensia Ilaria Parisi, Francesco Puoci
Sericin is a natural protein that has been used in biomedical and pharmaceutical fields as raw material for polypeptide-based drug delivery systems (DDSs). In this paper, it has been employed as pharmaceutical biopolymer for the production of sunitinib-polypeptide conjugate. The synthesis has been carried out by simple click reaction in water, using the redox couple l-ascorbic acid/hydrogen peroxide as a free radical grafting initiator. The bioconjugate molecular weight (50 kDa < Mw < 75 kDa) was obtained by SDS-PAGE, while the spectroscopic characteristics have been studied in order to reveal the presence of grafted sunitinib...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28181827/magnetically-triggered-drug-release-from-nanoparticles-and-its-applications-in-anti-tumor-treatment
#10
Xin Hua, Qin Yang, Zhimin Dong, Jiashuo Zhang, Wanjiang Zhang, Qiudong Wang, Shengnan Tan, Hugh D C Smyth
The objective of this study was to describe the magnetic nanoparticle-drug conjugates for improved control of drug delivery and drug release. The widely used anticancer agent Doxorubicin (DOX) was successfully conjugated via amine groups to the carboxylic functional groups coating magnetic nanoparticles (fluidMAG-CMX). Following purification of the nanoparticles, the conjugation of DOX on fluidMAG-CMX was confirmed using FTIR spectroscopy and confocal microscopy. The observed drug loading capacity of DOX was 22...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28181817/mathematical-modeling-of-intraperitoneal-drug-delivery-simulation-of-drug-distribution-in-a-single-tumor-nodule
#11
Margo Steuperaert, Giuseppe Falvo D'Urso Labate, Charlotte Debbaut, Olivier De Wever, Christian Vanhove, Wim Ceelen, Patrick Segers
The intraperitoneal (IP) administration of chemotherapy is an alternative treatment for peritoneal carcinomatosis, allowing for higher intratumor concentrations of the cytotoxic agent compared to intravenous administration. Nevertheless, drug penetration depths are still limited to a few millimeters. It is thus necessary to better understand the limiting factors behind this poor penetration in order to improve IP chemotherapy delivery. By developing a three-dimensional computational fluid dynamics (CFD) model for drug penetration in a tumor nodule, we investigated the impact of a number of key parameters on the drug transport and penetration depth during IP chemotherapy...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28165858/plga-nanoparticles-for-the-oral-delivery-of-nuciferine-preparation-physicochemical-characterization-and-in-vitro-in-vivo-studies
#12
Ying Liu, Xin Wu, Yushuai Mi, Bimeng Zhang, Shengying Gu, Gaolin Liu, Xiaoyu Li
This article reports a promising approach to enhance the oral delivery of nuciferine (NUC), improve its aqueous solubility and bioavailability, and allow its controlled release as well as inhibiting lipid accumulation. NUC-loaded poly lactic-co-glycolic acid nanoparticles (NUC-PLGA-NPs) were prepared according to a solid/oil/water (s/o/w) emulsion technique due to the water-insolubility of NUC. PLGA exhibited excellent loading capacity for NUC with adjustable dosing ratios. The drug loading and encapsulation efficiency of optimized formulation were 8...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28165834/seek-and-destroy-targeted-adeno-associated-viruses-for-gene-delivery-to-hepatocellular-carcinoma
#13
Bijay Dhungel, Aparna Jayachandran, Christopher J Layton, Jason C Steel
Hepatocellular carcinoma (HCC) is the most common form of primary liver cancer with high incidence globally. Increasing mortality and morbidity rates combined with limited treatment options available for advanced HCC press for novel and effective treatment modalities. Gene therapy represents one of the most promising therapeutic options. With the recent approval of herpes simplex virus for advanced melanoma, the field of gene therapy has received a major boost. Adeno-associated virus (AAV) is among the most widely used and effective viral vectors today with safety and efficacy demonstrated in a number of human clinical trials...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28165833/diclofenac-sodium-ion-exchange-resin-complex-loaded-melt-cast-films-for-sustained-release-ocular-delivery
#14
Goutham R Adelli, Sai Prachetan Balguri, Prakash Bhagav, Vijayasankar Raman, Soumyajit Majumdar
PURPOSE: The goal of the present study is to develop polymeric matrix films loaded with a combination of free diclofenac sodium (DFSfree) and DFS:Ion exchange resin complexes (DFS:IR) for immediate and sustained release profiles, respectively. METHODS: Effect of ratio of DFS and IR on the DFS:IR complexation efficiency was studied using batch processing. DFS:IR complex, DFSfree, or a combination of DFSfree + DFS:IR loaded matrix films were prepared by melt-cast technology...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28165823/nanocarriers-as-treatment-modalities-for-hypertension
#15
Tausif Alam, Saba Khan, Bharti Gaba, Md Faheem Haider, Sanjula Baboota, Javed Ali
Hypertension, a worldwide epidemic at present, is not a disease in itself rather it is an important risk factor for serious cardiovascular disorders including myocardial infarction, stroke, heart failure, and peripheral artery disease. Though numerous drugs acting via different mechanism of action are available in the market as conventional formulations for the treatment of hypertension but they face substantial challenges regarding their bioavailability, dosing and associated adverse effects which greatly limit their therapeutic efficacies...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28165822/in-vitro-and-in-vivo-investigation-for-optimization-of-niosomal-ability-for-sustainment-and-bioavailability-enhancement-of-diltiazem-after-nasal-administration
#16
H O Ammar, M Haider, M Ibrahim, N M El Hoffy
Diltiazem hydrochloride (DTZ) is a calcium channel antagonist depicted by extensive first pass metabolism and low oral bioavailability. The aim of this work was to develop niosomes for potential nasal delivery of DTZ. Niosomes protect hydrophilic drugs inside their core while nasal route offers both rapid onset and evasion of first-pass metabolism. Niosomes were prepared using a combination of Span 60 or Brij-52 with cholesterol (CHOL) in different molar ratios followed by determination of entrapment efficiency, particle size and in vitro drug release...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28165821/successful-delivery-of-docetaxel-to-rat-brain-using-experimentally-developed-nanoliposome-a-treatment-strategy-for-brain-tumor
#17
Tapan Kumar Shaw, Dipika Mandal, Goutam Dey, Murari Mohan Pal, Paramita Paul, Samrat Chakraborty, Kazi Asraf Ali, Biswajit Mukherjee, Amal Kumar Bandyopadhyay, Mahitosh Mandal
Docetaxel (DTX) is found to be very effective against glioma cell in vitro. However, in vivo passage of DTX through BBB is extremely difficult due to the physicochemical and pharmacological characteristics of the drug. No existing formulation is successful in this aspect. Hence, in this study, effort was made to send DTX through blood-brain barrier (BBB) to brain to treat diseases such as solid tumor of brain (glioma) by developing DTX-loaded nanoliposomes. Primarily drug-excipients interaction was evaluated by FTIR spectroscopy...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28165819/the-development-of-mechanically-formed-stable-nanobubbles-intended-for-sonoporation-mediated-gene-transfection
#18
Rodi Abdalkader, Shigeru Kawakami, Johan Unga, Yuriko Higuchi, Ryo Suzuki, Kazuo Maruyama, Fumiyoshi Yamashita, Mitsuru Hashida
In this study, stable nano-sized bubbles (nanobubbles [NBs]) were produced using the mechanical agitation method in the presence of perfluorocarbon gases. NBs made with perfluoropropane had a smaller size (around 400 nm) compared to that of those made with perfluorobutane or nitrogen gas. The lipid concentration in NBs affected both their initial size and post-formulation stability. NBs formed with a final lipid concentration of 0.5 mg/ml tended to be more stable, having a uniform size distribution for 24 h at room temperature and 50 h at 4 °C...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28165818/investigation-of-the-effect-of-solubility-increase-at-the-main-absorption-site-on-bioavailability-of-bcs-class-ii-drug-risperidone-using-liquisolid-technique
#19
Ahmed Khames
BCS class II drugs usually suffer inadequate bioavailability as dissolution step is the absorption rate limiting step. In this work, the effect of solubility increase at the main absorption site for these drugs was investigated using risperidone as a drug model. Liquisolid technique was applied to prepare risperidone per-oral tablets of high dissolution rate at intestinal pH (6.8) using versatile nonionic surfactants of high solubilizing ability [Transcutol HP, Labrasol and Labrasol/Labrafil (1:1) mixture] as liquid vehicles at different drug concentrations (10-30%) and fixed (R)...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28165817/pcm-and-tat-co-modified-liposome-with-improved-myocardium-delivery-in-vitro-and-in-vivo-evaluations
#20
Xin Wang, Hua Huang, Liangke Zhang, Yan Bai, Huali Chen
In this study, PCM and TAT co-modified liposome was developed as a novel drug carrier for myocardium delivery with evaluation of its in vitro and in vivo properties. Liposomes containing fluorescent probe coumarin-6 were prepared by thin-film hydration. The PCM ligands specifically bind to the PCM receptors in the extracellular connective tissue of primary myocardium cells (MCs), while the TAT ligands functioned as a classical cell penetrating peptide to make liposomes internalized by MCs. The unmodified liposome (L), PCM-modified liposome (PL), TAT-modified liposome (TL) and PCM and TAT co-modified liposome (PTL) were prepared and characterized...
November 2017: Drug Delivery
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